Assay Detail
Binding
CHEMBL4158682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of TRPC1/TRPC3/STIM1/Orai1 in HEK cells assessed as induction of store-operated calcium entry by measuring residual activity preincubated for 30 mins followed by tBhQ-mediated Ca2+ depletion and Ca2+ re-addition to extracellular solution measured for 600 secs by Fluo-4 AM-based fluorometric assay relative to control
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Short transient receptor potential channel 1 & 3/Stromal interaction molecule 1/Calcium release-activated calcium channel protein 1 (CHEMBL4296083) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.98 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL101896 | — | — | 1 | 6.52 |
| CHEMBL4177187 | — | — | 1 | 6.30 |
| CHEMBL4162723 | — | — | 1 | 6.22 |
| CHEMBL4162062 | — | — | 1 | 5.51 |
| CHEMBL4172741 | — | — | 1 | 5.36 |
| CHEMBL4173834 | — | — | 1 | - |
| CHEMBL4165917 | — | — | 1 | - |
| CHEMBL4160911 | — | — | 1 | - |
| CHEMBL4176117 | — | — | 1 | - |
| CHEMBL4164770 | — | — | 1 | - |
| CHEMBL4164404 | — | — | 1 | - |
| CHEMBL4165920 | — | — | 1 | - |
| CHEMBL4173839 | — | — | 1 | - |
| CHEMBL4169352 | — | — | 1 | - |
| CHEMBL4177191 | — | — | 1 | - |
| CHEMBL4159089 | — | — | 1 | - |
| CHEMBL4166992 | — | — | 1 | - |
| CHEMBL4162479 | — | — | 1 | - |
| CHEMBL4170397 | — | — | 1 | - |
| CHEMBL4161005 | — | — | 1 | - |
| CHEMBL4168931 | — | — | 1 | - |
| CHEMBL4170347 | — | — | 1 | - |
| CHEMBL4159717 | — | — | 1 | - |
| CHEMBL4166944 | — | — | 1 | - |
| CHEMBL4174834 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL101896 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4177187 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4162723 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4162062 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4172741 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4173834 | — | IC50 | - | — | - | |
| CHEMBL4165917 | — | IC50 | - | — | - | |
| CHEMBL4160911 | — | IC50 | - | — | - | |
| CHEMBL4176117 | — | IC50 | - | — | - | |
| CHEMBL4164770 | — | IC50 | - | — | - | |
| CHEMBL4164404 | — | IC50 | - | — | - | |
| CHEMBL4165920 | — | IC50 | - | — | - | |
| CHEMBL4173839 | — | IC50 | - | — | - | |
| CHEMBL4169352 | — | IC50 | - | — | - | |
| CHEMBL4177191 | — | IC50 | - | — | - | |
| CHEMBL4159089 | — | IC50 | - | — | - | |
| CHEMBL4166992 | — | IC50 | - | — | - | |
| CHEMBL4162479 | — | IC50 | - | — | - | |
| CHEMBL4170397 | — | IC50 | - | — | - | |
| CHEMBL4161005 | — | IC50 | - | — | - | |
| CHEMBL4168931 | — | IC50 | - | — | - | |
| CHEMBL4170347 | — | IC50 | - | — | - | |
| CHEMBL4159717 | — | IC50 | - | — | - | |
| CHEMBL4166944 | — | IC50 | - | — | - | |
| CHEMBL4174834 | — | IC50 | - | — | - |